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Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking Details. A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail. Not because the science is wrong. Not because the people aren’t brilliant. But because the program is run on duct tape and heroics instead of precision. Your program isn’t slipping because of bad science — it’s bleeding money because your systems were broken before the first experiment ran. And every time your Head of Biology spends each night copy-pasting data instead of thinking about the next experiment, your program is bleeding six figures in lost time and wasted salaries. Brilliant minds doing low impact work is not a strategy. It’s a slow-motion car crash. Hiring Won’t Save Your GPCR Drug Discovery Program When a drug discovery program stalls, the default reflex is always the same: hire more people. Bring in a computational chemist. Add a data scientist. Surely more hands will move the needle. But here’s the reality: even ultra-specialized experts can’t fix systemic dysfunction in their spare time. They’re hired for science, not for building operational scaffolding. And when you chain your highest-paid scientists to repetitive admin work, you’re not solving problems — you’re multiplying them. Every two-week delay in a DMTA cycle can burn through hundreds of thousands in salaries and overhead. That’s not a hiccup. That’s a hemorrhage. Bad Data Management Is Undermining Your GPCR Drug Discovery Team The real problem isn’t competence. It’s the absence of operational precision. Even flawless experiments collapse under sloppy systems. A few familiar failure points: Fragmented Data: GPCR programs spew data across files, folders, and inboxes. Without a unified drug discovery data management  pipeline, teams waste hours cleaning, reconciling, and integrating before they can even think about analysis. A good ELN that pipes instrument outputs into a central hub — where QC, analysis, consumption and consolidation across assays — isn’t a luxury. It’s oxygen. Undefined Protocols: “We’ll figure it out” is not a workflow. Without clear rules of engagement, communication becomes chaos, progress gets lost in Slack threads, and insights die in inboxes. Ambiguous Decision Gates: Molecules advance or stall based on vibes, not criteria. That leads to premature investment in weak scaffolds or endless tinkering with dead ends. These aren’t minor oversights. They’re cracks in the foundation. And cracks don’t stay small for long. Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn’t more people or shinier assays. It’s a deliberate blueprint for precision. This doesn’t mean an overnight overhaul. It means a commitment to continuous improvement — starting with the highest-friction gaps and working upward. Plan, fix at the root, and stop fighting the same fire every week. The payoff? Progress that’s predictable, not reactive. The Hidden Costs of Poor Drug Discovery Data Management Stop pretending more hires or new assays will save you. They won’t. Every DMTA cycle lost to fragmented data and sloppy processes costs your company hundreds of thousands of dollars. That’s not “part of the process.” That’s a chaos tax — and you’re paying it in cash, time, and morale. If you want your program to survive, you need a Blueprint for Precision. Not next quarter. Not after the next fire drill. Now. Because the truth is harsh: in drug discovery, you don’t run out of science. You run out of money. And if your systems aren’t built for precision, you’ll run out fast. 👉 In Part 2, we’ll expose exactly how fragmented data cripples GPCR programs — and how to fix it before it sinks yours. And if you’re already seeing the cracks? Don’t wait for Part 2. Reach out. Let’s build the systems now, before the next delay burns another half a million. 🚀 Book your free 30-minute precision audit — before your next DMTA cycle costs another $200K Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉   Yamina.org

How the Mass Action Law underpins nearly every model Future of Receptor Theory: Linkage vs.

Push the boundaries  of receptor pharmacology and its real-world applications. They’re already behind blockbuster drugs: GLP-1 receptor agonists  – reshaping obesity & type 2 diabetes Dopamine D2 receptor modulators  – transforming treatment for Parkinson’s & schizophrenia. Serotonin & dopamine receptor modulation  for neuropsychiatric disorders. Kenakin’s work on functional selectivity  has transformed GPCR drug discovery, showing how to bias receptor

Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo signalling repertoire Common to all cytomegalovirus (CMV) genomes analysed to date is the presence of G protein-coupled receptors (GPCR). Constitutive G protein-coupled M33 signalling is required for these phenotypes, although the contribution IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle production and circulation of vasoconstrictors, resulting in enhanced signalling through their cognate G protein-coupled receptors (GPCR). GPCR signalling through phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) promotes VSMC proliferation In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are

Why I Started GPCR Consulting You've got great data. You've got brilliant scientists. But your GPCR program still isn't moving at the pace it should. I've seen this pattern unfold across biotech, academia, and nonprofits. The assays are running, data is flowing in from your CROs or your internal labs , yet progress stalls. Decisions are slow, crucial data is siloed, and despite everyone working hard, programs drift. For over two decades, my work has centered on GPCR pharmacology . In every role and sector, I found myself drawn to the same critical challenges: missed opportunities, misaligned systems, and promising programs stalling despite strong science. I was always the one identifying what could be improved: The essential structure that was missing. The clarity that was desperately lacking. The unnecessary friction that slowed everything down. Traditional roles rarely gave me the freedom to implement these changes at the scale needed. So, I created a new path—one that allows me to embed, optimize, and accelerate GPCR programs from the inside out. The GPCR Data Dilemma: The Lego Bucket Problem I've seen promising GPCR programs generate massive volumes of high-quality data. But without structure, it's just a messy pile of colored blocks. I call this the Lego Bucket Problem . You have the data, but not the definitive direction. This disconnect frequently leads to: Underperforming assays. Internal data and CRO outputs  misaligned with strategic goals. Delays in critical go/no-go decisions. Frustrated teams and slipping timelines. It's not just a scientific issue—it's an operational one. You can't move fast without clarity, and you can't make confident decisions without robust structure. My Approach: Biology, Execution, Systems My consulting approach uniquely blends deep pharmacology expertise with the operational discipline required to make that expertise actionable. Here's how I bring a fresh perspective: Biology-First, Data-Driven Strategy:  I help you focus on the science that truly matters. We cut through the noise, elevate what's working, and strategically solve what's not, ensuring your GPCR program stays on target. Embedded Execution:  I work alongside your team—not above it. I'll help write CRO scopes, meticulously review assay data, flag risks early, and keep your programs relentlessly on track. Systems That Drive Progress:  From assay tracking to data workflows, I design simple, scalable tools that surface insights early and dramatically reduce delays, transforming your data into actionable intelligence. A Broader Lens: Dr. GPCR As the co-founder of Dr. GPCR, we've built a global hub connecting over 1,300 GPCR scientists dedicated to this field. These ongoing conversations keep me on the front lines, sharpening my understanding of the common bottlenecks and evolving needs across the entire GPCR community. My Consulting Philosophy This practice is built on three core values: Scientific Integrity:  Every recommendation is grounded in real-world evidence and extensive experience. Operational Discipline:  Robust systems and clear structure aren't "nice to have"—they are absolutely essential for efficient progress. Collaborative Partnership:  I embed, contribute, and build solutions hand-in-hand with your team. Ready to Move Your GPCR Program Forward? If you're navigating a stuck GPCR program, planning your next crucial milestone, or struggling to gain clarity from complex data, I'd love to help. 📌 Learn more about my services: Yamina.org 📅 Book a 30-minute strategy call: https://calendly.com/drgpcr/yamina-corner

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic analysis and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR) signaling The kinase GRK2 and the multifunctional scaffolding protein β-arrestin2 are key integrated signaling

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early (Daphnia magna) reveals a high level of orthological relationship of amine, neuropeptide, and opsin receptor repertoire, while purinergic and chemokine receptors were highly differentiated in humans.

Calcium (Ca2+) signaling is known to direct processes that govern chondrocyte gene expression, protein One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs that long-term CNO stimulatory culture have on hM3Dq [Ca2+]i signaling dynamics, proliferation, and protein This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

G Protein-Coupled Receptors: A Century of Research and Discovery. Allosteric modulation of G protein-coupled receptor signaling. Endogenous allosteric modulators of G protein-coupled receptors. Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling. Mini G protein probes for active G protein-coupled receptors (GPCRs) in live cells.

Excited to hear Dr. Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe

October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system , L-glutamate, and mGlu5 receptor activity can be allosterically modulated by negative or positive allosteric The mGlu5 receptor is a promising target for the treatment of psychiatric and neurodegenerative diseases

GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through Mitogen-Activated Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor (GPCR) GPR183 harvested at the time of peak hypersensitivity implicate potential contributions of mitogen-activated protein

counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical on the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling."

conformational consequences of the differential activity of cannabidiol with two endocannabinoid-activated G-protein-coupled receptors "Cannabidiol (CBD), the major non-psychoactive phytocannabinoid present in the plant Cannabis belong to the family of G-protein-coupled receptors (GPCRs). investigate the interacting determinants of CBD in two closely related endocannabinoid-activated GPCRs, the G-protein-coupled receptor 55 (GPR55) and the cannabinoid type 1 receptor (CB1).

The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors Several S1PR therapeutic drugs have been developed to treat these diseases; however, they lack receptor In this article, we describe a 2.2 Å resolution room temperature crystal structure of the human S1P5 receptor demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies the receptor

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor Agonist activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor Eliminating β2AR S-nitrosylation by mutation of C265 augments β2AR protein kinase A signaling, enables β2AR nitric oxide (NO) signaling, renders mice resistant to bronchoconstriction, and protects mice from

Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR This emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate (f) the presence of CaSR autoantibodies that operated as biased allosteric modulators of CaSR, and (g) Our observations with these prominent commonalities may provide new insights into the phenotype and characteristics

2022 Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors "Neural network (NN)-based protein modeling methods have improved significantly in recent G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous This work directly compares the performance of these novel deep learning-based protein modeling methods We collected the experimentally determined structures of 73 GPCRs from the Protein Data Bank.

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein In contrast to Gpr3-deficient mice, G protein-biased GPR3 mice do not display elevated anxiety levels We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease glial response that may limit amyloid plaque development in G protein-biased GPR3 AD mice. Collectively, these studies indicate that GPR3-mediated G protein and β-arrestin signaling produce discrete

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway PKA facilitates the actions of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR) to modulate cAMP levels.

October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In the former, stimulation of Gs-coupled receptors leads to increases in contractility, whereas stimulation of Gq-coupled receptors modulates cellular survival and hypertrophic responses. associated signaling machinery are localized in these cells with an emphasis on nuclear membrane-localized receptors

October 2022 Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of Adhesion Receptor GPR97 "Adhesion G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play The orphan receptor GPR97, activated by glucocorticoid stress hormones, is a prototypical aGPCR. Although it has been established that the palmitoylation of the C-terminal Go protein is essential for only allosterically strengthens the internal interactions between Gαo and Gβγ, but also enhances the coupling

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that

Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs) are the largest family of human proteins. They have a common structure and, signaling through a much smaller set of G proteins, arrestins, and We also discovered that no single receptor drives this pattern, but rather multiple receptors contain Phenotypic characterization suggests these mutations induce perturbation of G protein activation and/

Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic